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Ophthalmic Drug Delivery Systems

Ophthalmic Drug Delivery Systems

Ophthalmic drug delivery faces major limitations due to poor absorption across the corneal membrane. This process is primarily driven by diffusion and is influenced by two main factors: the physicochemical properties of the drug and tear drainage. Most ophthalmic drugs, such as pilocarpine, epinephrine, atropine, and local anesthetics, are weak bases. They are typically formulated at an acidic pH to enhance chemical stability. However, this leads to high ionization, reducing their ability to...

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Combination of Microstereolithography and Electrospinning to Produce Membranes Equipped with Niches for Corneal Regeneration

Combination of Microstereolithography and Electrospinning to Produce Membranes Equipped with Niches for Corneal Regeneration

Published on: September 12, 2014

Development of Innovative Electrospun Nepafenac-Loaded Nanofibers-based Ophthalmic Inserts.

Safaa Omer¹, Nándor Nagy², Emőke Szőcs²

¹University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Street 7-9, H-1092 Budapest, Hungary.

International Journal of Pharmaceutics

|November 4, 2024

Summary

Electrospun nanofibrous webs offer a promising approach for ocular nepafenac delivery. These webs demonstrate good solubility, stability, and corneal distribution, suggesting potential for ophthalmic inserts.

Keywords:

Nepafenac-loaded formulations accelerated stability test cytocompatibility study electrospun nanofiber-based ocular insert ex vivo permeability study in vitro dissolution study morphological and solid-state characterization

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Area of Science:

Materials Science
Pharmaceutical Sciences
Ophthalmology

Background:

Electrospun nanofibers offer potential for patient-centric ophthalmic formulations.
Improving solubility and stability of drugs like nepafenac is crucial for ocular delivery.

Purpose of the Study:

To develop and investigate 0.1% w/w nepafenac-loaded electrospun nanofibrous webs for ocular delivery.
To assess physicochemical properties, drug release, permeability, and cytocompatibility.

Main Methods:

Nine different nepafenac formulations were prepared using electrospinning.
Characterization included scanning electron microscopy, FTIR, XRD, drug release studies, and in vitro/ex vivo permeability assays.
Cytocompatibility was evaluated using the chick embryo chorioallantoic membrane model.

Main Results:

Fibrous morphology confirmed by SEM; FTIR and XRD indicated polymer cross-linking and amorphous solid dispersion.
All formulations exhibited complete and rapid nepafenac release (≤ 60 minutes) following first-order kinetics.
Formulations F3, F6, and F9 showed significant in vitro and ex vivo permeability, with comparable corneal distribution to a commercial suspension.

Conclusions:

Developed nepafenac-loaded nanofiber webs are stable under stress conditions and exhibit good cytocompatibility.
These nanofiber webs represent a promising candidate for advanced ophthalmic inserts for ocular nepafenac delivery.